590368-25-5
590368-25-5 structure
- Name: WX 671
- Chemical Name: Upamostat
- CAS Number: 590368-25-5
- Molecular Formula: C32H47N5O6S
- Molecular Weight: 629.81000
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Ser/Thr Protease
- Create Date: 2016-07-10 10:26:43
- Modify Date: 2024-01-17 16:12:09
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Upamostat is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor.
| Name | Upamostat |
|---|---|
| Synonyms |
WX 671
1-Piperazinecarboxylic acid,4-((2S)-3-(3-((hydroxyamino)iminomethyl)phenyl)-1-oxo-2-(((2,4,6-tris(1-methylethyl)phenyl)sulfonyl)amino)propyl)-,ethyl ester 4-[(2S)-3-[3-[(Hydroxyamino)iminomethyl]phenyl]-1-oxo-2-[[[2,4,6-tris(1-methylethyl)phenyl]sulfonyl]amino]propyl]-1-piperazinecarboxylic acid ethyl ester ethyl 4-[(2S)-3-[3-[(E)-(hydroxyhydrazinylidene)methyl]phenyl]-2-[[2,4,6-tri(propan-2-yl)phenyl]sulfonylamino]propanoyl]piperazine-1-carboxylate |
| Description | Upamostat is a serine protease inhibitor. Upamostat is the orally available prodrug of the WX-UK1, which is a urokinase plasminogen activator (uPA) inhibitor. |
|---|---|
| Related Catalog | |
| Target |
Serine protease, uPA[1] |
| In Vitro | Upamostat is the urokinase plasminogen activator (uPA) inhibitor. Upamostat is the oral pro-drug of the active metabolite WX-UK1, a novel uPA inhibitor[1]. Upamostat inhibits the urokinase-type plasminogen activator (uPA) system, which plays a major role in tumor invasion and metastasis. Upamostat is the orally available amidoxime- (i.e. hydroxyamidine-) prodrug of the pharmacologically active form, WX-UK1[2]. |
| In Vivo | The validated method is used to evaluate the pharmacokinetics of Upamostat (Mesupron) in rats. The mean plasma concentrations of Upamostat after a single intravenous injection of 2 mg/kg in five rats are measured. The substance decays in a mono-phasic pattern with a terminal half-life of 0.5 h; its volume of distribution is 2.0 L/kg, and clearance is about 2.7 L/h/kg[3]. |
| Animal Admin | Rats[3] Five 9-week old Sprague-Dawley rats are administered a single intravenous injection of 2 mg/kg of Upamostat. Upamostat is dissolved in a mixture of normal saline, dimethylacetamide, polyethylene glycol 400 and DMSO (3:3:3:1). Blood samples (0.15 mL) are taken serially for up to 10 h after drug administration and collected in heparinized centrifuge tubes. After centrifugation at 13,200 rpm for 10 min, the plasma samples are analyzed[3]. |
| References |
| Density | 1.25 |
|---|---|
| Molecular Formula | C32H47N5O6S |
| Molecular Weight | 629.81000 |
| Exact Mass | 629.32500 |
| PSA | 149.02000 |
| LogP | 6.29820 |
| Storage condition | 2-8℃ |